论文部分内容阅读
丝虫病临床用药目前仍以海群生为主,对微丝蚴效果显著,对成虫作用不明显,无根治疗效。根据硝基咪唑类衍生物具有抗蠕虫作用,故合成了具有下列通式Ⅰ的硝基咪唑类衍生物41个,由中国医学科学院寄生虫病研究所筛选。初步药理实验结果发现其中有9个化合物在感染棉鼠丝虫的棉鼠体内有明显的抗虫活性。其中以2-甲基-5-硝基咪唑-1-乙醇(Ⅱ_1;即是灭滴灵)及2-甲基-5-硝基咪唑-1-氯乙烷(Ⅰ_2)两个化合物对成虫有较强的杀灭作用(详见表1)。
Clinical application of filariasis is still mainly based on sea quiz, the effect of microfilariae significantly, the role of adults is not obvious, no cure. Based on the anthelmintic effect of nitroimidazole derivatives, 41 nitroimidazole derivatives having the following general formula I were synthesized and screened by the Institute of Parasitic Diseases, Chinese Academy of Medical Sciences. Preliminary pharmacological experiments found that there are nine compounds in cotton wool infected mice in vivo significant anti-insect activity. Among them, two compounds, 2-methyl-5-nitroimidazole-1-ethanol (Ⅱ_1; metronidazole) and 2-methyl-5-nitroimidazole- Have a strong killing effect (see Table 1).